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Relistor

METHYLNALTREXONE BROMIDE

Manufacturer: Salix Pharmaceuticals, Inc.

Score: 141.0

Quick Summary

Relistor (methylnaltrexone bromide) is a mu-opioid receptor antagonist used for the treatment of opioid-induced constipation (OIC) in adults with chronic non-cancer pain and advanced illness. It works by decreasing the constipating effects of opioids without impacting opioid-mediated analgesic effects on the central nervous system. The recommended dosage is 450 mg once daily in the morning for OIC in adult patients with chronic non-cancer pain, and 12 mg subcutaneously once daily for OIC in adult patients with advanced illness. Relistor is contraindicated in patients with known or suspected gastrointestinal obstruction and patients at increased risk of recurrent obstruction. Common adverse reactions include abdominal pain, diarrhea, and nausea.

Key Clinical Findings and Indications

  • Treatment of opioid-induced constipation (OIC) in adults with chronic non-cancer pain
  • Treatment of OIC in adults with advanced illness
  • Mu-opioid receptor antagonist
  • Decreases constipating effects of opioids without impacting opioid-mediated analgesic effects

Important Safety Information

Warning

Gastrointestinal perforation, severe or persistent diarrhea, and opioid withdrawal

Contraindications

  • Known or suspected gastrointestinal obstruction
  • Patients at increased risk of recurrent obstruction

Adverse Reactions

  • Abdominal pain
  • Diarrhea
  • Nausea
  • Vomiting
  • Hyperhidrosis
  • Anxiety
  • Muscle spasms
  • Rhinorrhea
  • Chills

Dosing Recommendations

General Guidance

Dosage adjustments may be necessary in patients with renal or hepatic impairment

OIC in adult patients with chronic non-cancer pain

Adult Dose

450 mg once daily in the morning

Pediatric Dose

Not established

OIC in adult patients with advanced illness

Adult Dose

12 mg subcutaneously once daily

Pediatric Dose

Not established

Special Population Considerations

Pregnancy

  • Limited data available
  • Use with caution
  • May precipitate opioid withdrawal in fetus

Nursing Mothers

  • Not studied
  • Use with caution

Pediatric Use

  • Not established
  • Juvenile animal studies showed adverse effects

Geriatric Use

  • No overall differences in effectiveness or safety
  • Monitor for adverse reactions